阿司匹林包合物微孔渗透泵片制备及释药机制考察

聂琴 ,  吴静澜 ,  罗坤顺 ,  徐剑 ,  张永萍 ,  傅建

科学技术与工程 ›› 2025, Vol. 25 ›› Issue (1) :84-93

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科学技术与工程 ›› 2025, Vol. 25 ›› Issue (1) :84-93 DOI: 10.12404/j.issn.1671-1815.2307868
医药、卫生

阿司匹林包合物微孔渗透泵片制备及释药机制考察

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Preparation and Release Mechanism of Aspirin Inclusion Micro-porous Osmotic Pump Tablets

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摘要

依次采用单因素试验和Box-Behnken设计结合响应面法,以释放度为评价指标,优化了阿司匹林包合物微孔渗透泵片的最佳制备工艺。首先制备β-环糊精阿司匹林包合物,再以醋酸纤维素为包衣材料、聚乙二醇4000为致孔剂制备阿司匹林包合物微孔渗透泵片。体外释放度试验表明,该工艺制备的阿司匹林包合物微孔渗透泵片与市售阿司匹林肠溶片在人工胃液中0~2 h内累积释放率分别为1.5%和1.6%;将释放介质调至pH 6.8后,两种剂型在10 h时的累积释药量无显著差异。此外,该包合物微孔渗透泵片在12 h内呈现零级释放且释放较完全(累积释放率>90%),提示有可能减轻药物对胃黏膜的损伤。

Abstract

The Box-Behnken experimental design and response surface methodology were employed to optimize the preparation of the aspirin micro-porous osmotic pump tablets. The core of the tablet was prepared with aspirin and β-CD inclusion, then osmotic pump tablets were obtained by coating a layer of cellulose acetate containing PEG 4000 as porogenic agent. The in vitro release test shows that the aspirin inclusion complex microporous osmotic pump tablets prepared by this process has a cumulative release rate of 1.5% and 1.6% within 0~2 h in artificial gastric juice compared to commercially available aspirin enteric coated tablets. After adjusting the release medium to pH 6.8, there is no significant difference in the cumulative drug release between the two formulations at 10 h. And the inclusion complex microporous osmotic pump tablet shows zero order release and complete release within 12 h(cumulative release rate > 90%), indicating the possibility of reducing drug damage to the gastric mucosa.

关键词

阿司匹林 / 微孔渗透泵片 / 星点设计 / 释药机制

Key words

aspirin / microporous osmotic pump tablet / central composite design / release mechanism

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聂琴, 吴静澜, 罗坤顺, 徐剑, 张永萍, 傅建. 阿司匹林包合物微孔渗透泵片制备及释药机制考察[J]. 科学技术与工程, 2025, 25(1): 84-93 DOI:10.12404/j.issn.1671-1815.2307868
NIE Qin, WU Jing-lan, LUO Kun-shun, XU Jian, ZHANG Yong-ping, FU Jian. Preparation and Release Mechanism of Aspirin Inclusion Micro-porous Osmotic Pump Tablets[J]. Science Technology and Engineering, 2025, 25(1): 84-93 DOI:10.12404/j.issn.1671-1815.2307868

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基金资助

贵阳市高层次创新型青年科技人才(筑科合同[2021]43-10)

贵州省(第六批)高层次创新型人才(“千”层次)

贵州省高层次创新型人才(黔科合平台人才-GCC[2023]037)

国家苗药工程技术研究中心能力提升(黔科合中引地[2023]006)

贵州省教育厅滚动支持省属高校科研平台团队(黔教技[2022]022)

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